1. A novel orally active inhibitor of HLE.
- Author
-
Varga M, Kapui Z, Bátori S, Nagy LT, Vasvári-Debreczy L, Mikus E, Urbán-Szabó K, and Arányi P
- Subjects
- Administration, Oral, Animals, Asthma chemically induced, Asthma drug therapy, Asthma pathology, Cyclic S-Oxides chemistry, Cyclic S-Oxides metabolism, Cystic Fibrosis chemically induced, Cystic Fibrosis drug therapy, Cystic Fibrosis pathology, Dose-Response Relationship, Drug, Enzyme Inhibitors chemistry, Enzyme Inhibitors metabolism, Hemorrhage chemically induced, Hemorrhage drug therapy, Hemorrhage pathology, Humans, Inflammation chemically induced, Inflammation drug therapy, Inflammation pathology, Leukocyte Elastase administration & dosage, Leukocyte Elastase metabolism, Lung Diseases, Obstructive chemically induced, Lung Diseases, Obstructive drug therapy, Lung Diseases, Obstructive pathology, Mice, Models, Chemical, Pulmonary Emphysema chemically induced, Pulmonary Emphysema drug therapy, Pulmonary Emphysema pathology, Thiazoles chemistry, Thiazoles metabolism, Cyclic S-Oxides pharmacology, Enzyme Inhibitors pharmacology, Leukocyte Elastase antagonists & inhibitors, Thiazoles pharmacology
- Abstract
Human leukocyte elastase (HLE) is a serine proteinase, capable of degrading a variety of structural matrix proteins. SSR69071 2-[(4-isopropyl-6-methoxy-1,1-dioxido-3-oxo-1,2-benzisothiazol-2(3H)-yl)methoxy]-9-(2-piperidin-1-ylethoxy)-4H-pyrido[1,2-a]pyrimidin-4-one was selected as a novel orally active HLE inhibitor for treatment of chronic obstructive pulmonary diseases, asthma, emphysema, cystic fibrosis and several inflammatory diseases (WO 01/44245 A1) (J. Pharm. Exp. Ther., submitted for publication).
- Published
- 2003
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